Properties
一种具有生物活性的小分子多激酶抑制剂，具有抗肿瘤活性，抑制Aurora A/B，Ki分别为8.0 nM和9.2 nM。
CYC116 is an orally bioavailable small molecule multi-kinase inhibitor with antineoplastic activity. Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. Aurora kinases are serine/threonine protein kinases that are only expressed in actively dividing cells and are critical in division or mitosis. VEGFR2 is a receptor tyrosine kinase that appears to account for most of the mitogenic and chemotactic effects of vascular endothelial growth factor (VEGF) on adult endothelial cells.
CYC116是一种具有抗肿瘤活性的口服生物利用型小分子多激酶抑制剂。 Aurora激酶/ VEGFR 2抑制剂CYC116抑制Aurora激酶A和B和血管内皮生长因子受体2（VEGFR2），导致细胞周期中断，细胞快速死亡和血管生成抑制。 极光激酶是丝氨酸/苏氨酸蛋白激酶，仅在活跃分裂的细胞中表达，对分裂或有丝分裂至关重要。 VEGFR2是一种酪氨酸激酶，似乎可以解释血管内皮生长因子（VEGF）对成年内皮细胞的大部分促有丝分裂和趋化作用。
| Iupac Name | 4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine |
| Inchi Code | 1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23) |
| Inchi Key | GPSZYOIFQZPWEJ-UHFFFAOYSA-N |
Description
| Synonym | 4-methyl-5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)thiazol-2-amine |
| Purity | 99% |
安全信息
RIDADR NONH for all modes of transport
